| Chemical Properties | Back Directory | [Boiling point ]
499.4±55.0 °C(Predicted) | [density ]
1.28±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
-5.02±0.60(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
CPI-4203 is a selective inhibitor of KDM5 demethylases, structurally related to CPI 455. The KDM5 family of histone demethylases catalyzes the demethylation of histone H3 on lysine 4 (H3K4) and is required for the survival of drug-tolerant persister cancer cells (DTPs). | [Uses]
CPI-4203 is a potent KDM5A inhibitor with an IC50 of 250 nM. CPI-4203 is competitive with 2-oxoglutarate (2-OG). CPI-4203 is structurally related to CPI-455 (HY-100421) but is less potent[1]. | [References]
[1] Vinogradova M, et al. An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells. Nat Chem Biol. 2016 Jul;12(7):531-8. DOI:10.1038/nchembio.2085 |
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BOC Sciences
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https://www.bocsci.com |
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